IE821365L - Androstanes - Google Patents

Androstanes

Info

Publication number
IE821365L
IE821365L IE821365A IE136582A IE821365L IE 821365 L IE821365 L IE 821365L IE 821365 A IE821365 A IE 821365A IE 136582 A IE136582 A IE 136582A IE 821365 L IE821365 L IE 821365L
Authority
IE
Ireland
Prior art keywords
compounds
alkyl
carbon atoms
group
blocking
Prior art date
Application number
IE821365A
Other versions
IE53463B1 (en
Original Assignee
Akzo Nv
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Akzo Nv filed Critical Akzo Nv
Publication of IE821365L publication Critical patent/IE821365L/en
Publication of IE53463B1 publication Critical patent/IE53463B1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J13/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
    • C07J13/005—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17 with double bond in position 16 (17)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0003—Androstane derivatives
    • C07J1/0011—Androstane derivatives substituted in position 17 by a keto group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0003—Androstane derivatives
    • C07J1/0018—Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa
    • C07J1/0022—Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J21/005—Ketals
    • C07J21/008—Ketals at position 17
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005—Oxygen-containing hetero ring
    • C07J71/001—Oxiranes

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Neurology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

This invention relates to novel mono- and bisquaternary ammonium derivatives of 5 alpha -androstanes having the formula: <IMAGE> wherein: R1=H or alkyl (1-4 C); R2 and R3 each are alkyl (1-4 C) or form together with the N-atom a piperidino, pyrrolidino or morpholino group; R4=O or H( beta OR5) and R5=H or acyl derived from an organic carboxylic acid having 1-18, preferably 1-6 carbon atoms; the quaternarizing group being a saturated or unsaturated aliphatic hydrocarbon group having 1-4 carbon atoms the anion being halide; and acid addition salts of the monoquaternary compounds; and to pharmaceutical preparations containing one or more of said androstane compounds as active constituent. The compounds according to the invention are non-depolarizing neuromuscular blocking agents having very quick onset and recovery characteristics, a short duration of action and a favorable dissociation between muscle blocking and vagal blocking effects. [US4447425A]
IE1365/82A 1981-06-15 1982-06-08 Mono-and bisquaternary ammonium derivatives of 2 beta,16 beta-d-amino-5 alpha-androstane derivatives and pharmaceutical preparations containing same IE53463B1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GB8118365 1981-06-15

Publications (2)

Publication Number Publication Date
IE821365L true IE821365L (en) 1982-12-15
IE53463B1 IE53463B1 (en) 1988-11-23

Family

ID=10522526

Family Applications (1)

Application Number Title Priority Date Filing Date
IE1365/82A IE53463B1 (en) 1981-06-15 1982-06-08 Mono-and bisquaternary ammonium derivatives of 2 beta,16 beta-d-amino-5 alpha-androstane derivatives and pharmaceutical preparations containing same

Country Status (11)

Country Link
US (1) US4447425A (en)
EP (1) EP0067480B1 (en)
JP (1) JPS5813600A (en)
AU (1) AU551427B2 (en)
CA (1) CA1186681A (en)
DE (1) DE3261364D1 (en)
DK (1) DK268382A (en)
ES (1) ES513088A0 (en)
FI (1) FI72731C (en)
HU (1) HU186074B (en)
IE (1) IE53463B1 (en)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5804576A (en) * 1983-08-02 1998-09-08 Research Corporation Technologies, Inc. Derivatives of 5-androsten-17-ones and 5-androstan-17-ones
ES8706717A1 (en) * 1983-08-02 1987-07-01 Research Corp Steroids and therapeutic compositions containing same.
US5656621A (en) * 1983-08-02 1997-08-12 Research Corporation Tech., Inc. Steroids useful as anti-cancer and anti-obesity agents
US5714481A (en) * 1983-08-02 1998-02-03 Research Corporation Technologies, Inc. Derivatives of 5-androsten-17 ones and 5-androstan-17-ones
GB8708886D0 (en) * 1987-04-14 1987-05-20 Akzo Nv 2beta-morpholino-androstane derivatives
GB8804579D0 (en) * 1988-02-26 1988-03-30 Akzo Nv Novel 16-homo-piperidino-androstane derivatives & processes for their preparation
DE4232656C2 (en) * 1992-09-29 1995-01-12 Sigma Tau Ind Farmaceuti Cyclopentane perhydrophenanthrene-17-furyl-3β derivatives, processes for their preparation and pharmaceutical compositions containing them
CZ300694A3 (en) * 1993-12-02 1996-05-15 Akzo Nobel Nv Substituted 2beta-morpholinandrostane derivatives, process of their preparation, their use for preparing pharmaceutical preparations and pharmaceutical compositions containing thereof
IT1277700B1 (en) * 1995-12-22 1997-11-11 Poli Ind Chimica Spa PROCESS OF PREPARATION OF 2-BETA, 16-BETA-DIAMINO 3-ALPHA, 17-BETA-DIACYLOSS 5-ALPHAANDROSTANS, STRUCTURED NEUROMUSCULAR BLOCKERS
KR20070085703A (en) * 2005-09-13 2007-08-27 시코르, 인크. Process for the synthesis of rocuronium bromide

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1138605A (en) * 1965-02-19 1969-01-01 Organon Labor Ltd Improvements in or relating to new 2-ß,16-ß-diamino-androstanes
GB1454749A (en) * 1972-11-29 1976-11-03 Akzo Nv 2beta, 16beta-diamino-androstanes and their preparation
EP0008824B1 (en) * 1978-09-05 1982-04-28 Akzo N.V. Acid addition salts of 16-beta-monoquaternary ammonium derivatives of 2-beta, 16-beta-bis-piperidino-androstanes and pharmaceutical preparations containing same
IE50675B1 (en) * 1979-12-12 1986-06-11 Akzo Nv Bis-and mono-quaternary ammonium derivatives of 2beta,16beta-dipiperidino-5alpha-androstanes,processes for their preparation and pharmaceutical preparations

Also Published As

Publication number Publication date
JPS5813600A (en) 1983-01-26
JPH0249320B2 (en) 1990-10-29
IE53463B1 (en) 1988-11-23
DK268382A (en) 1982-12-16
CA1186681A (en) 1985-05-07
ES8308889A1 (en) 1983-08-16
FI72731B (en) 1987-03-31
HU186074B (en) 1985-05-28
FI822131A0 (en) 1982-06-14
DE3261364D1 (en) 1985-01-10
US4447425A (en) 1984-05-08
ES513088A0 (en) 1983-08-16
AU8483882A (en) 1982-12-23
FI72731C (en) 1987-07-10
EP0067480B1 (en) 1984-11-28
AU551427B2 (en) 1986-05-01
EP0067480A1 (en) 1982-12-22

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